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National Cancer Institute
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Version: 17.06d (Release date: 2017-06-26)
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Cobimetinib (Code C68923)

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Terms & Properties

Preferred Name: Cobimetinib

Definition: An orally bioavailable small-molecule inhibitor of mitogen-activated protein kinase kinase 1 (MAP2K1 or MEK1), with potential antineoplastic activity. Cobimetinib specifically binds to and inhibits the catalytic activity of MEK1, resulting in inhibition of extracellular signal-related kinase 2 (ERK2) phosphorylation and activation and decreased tumor cell proliferation. Preclinical studies have demonstrated that this agent is effective in inhibiting the growth of tumor cells bearing a B-RAF mutation, which has been found to be associated with many tumor types. A threonine-tyrosine kinase and a key component of the RAS/RAF/MEK/ERK signaling pathway that is frequently activated in human tumors, MEK1 is required for the transmission of growth-promoting signals from numerous receptor tyrosine kinases.

Display Name: Cobimetinib

Label: Cobimetinib

NCI Thesaurus Code: C68923 (Search for linked caDSR metadata)  (search value sets)

NCI Metathesaurus Link: C2346910  (see NCI Metathesaurus info)

Synonyms & Abbreviations: (see Synonym Details)
Cobimetinib
COBIMETINIB
Cotellic
GDC-0973
MEK Inhibitor GDC-0973
XL518

External Source Codes: 
FDA UNII Code ER29L26N1X
PDQ Closed Trial Search ID 551654
PDQ Open Trial Search ID 551654 (check for NCI PDQ open clinical trial info)
UMLS CUI C2346910

Other Properties:
     Name Value (qualifiers indented underneath)
code C68923
Contributing_Source CTRP
Contributing_Source FDA
Legacy_Concept_Name MEK_Inhibitor_XL518
Semantic_Type Pharmacologic Substance

Additional Concept Data: 
Defined Fully by Roles: No  

URL: https://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C68923

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